Literature DB >> 12270155

Development of potent and selective dipeptidyl peptidase II inhibitors.

Kristel Senten1, Pieter Van der Veken, Gunther Bal, Ingrid De Meester, Anne-Marie Lambeir, Simon Scharpé, Brigitte Bauvois, Achiel Haemers, Koen Augustyns.   

Abstract

Structure-activity investigations of product-like dipeptide analogues lacking the C-terminal carbonyl function resulted in potent and selective dipeptidyl peptidase II (DPP II) inhibitors. Dab-Pip has an IC(50)=0.13 microM for DPP II and a 7600-fold selectivity with respect to DPP IV. This compound will be highly valuable for the investigation of the biochemical function of DPP II.

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Year:  2002        PMID： 12270155     DOI： 10.1016/s0960-894x(02)00603-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  The metabolic serine hydrolases and their functions in mammalian physiology and disease.

Authors:  Jonathan Z Long; Benjamin F Cravatt
Journal:  Chem Rev       Date:  2011-06-23       Impact factor: 60.622

2.  Kinetic investigation of human dipeptidyl peptidase II (DPPII)-mediated hydrolysis of dipeptide derivatives and its identification as quiescent cell proline dipeptidase (QPP)/dipeptidyl peptidase 7 (DPP7).

Authors:  Marie-Berthe Maes; Anne-Marie Lambeir; Kambiz Gilany; Kristel Senten; Pieter Van der Veken; Barbara Leiting; Koen Augustyns; Simon Scharpé; Ingrid De Meester
Journal:  Biochem J       Date:  2005-03-01       Impact factor: 3.857

3.  Catalytic properties and inhibition of proline-specific dipeptidyl peptidases II, IV and VII.

Authors:  Barbara Leiting; KellyAnn D Pryor; Joseph K Wu; Frank Marsilio; Reshma A Patel; Charles S Craik; Jonathan A Ellman; Richard T Cummings; Nancy A Thornberry
Journal:  Biochem J       Date:  2003-04-15       Impact factor: 3.857

4.  Dipeptidyl peptidase IV, aminopeptidase N and DPIV/APN-like proteases in cerebral ischemia.

Authors:  Peter Röhnert; Werner Schmidt; Patrick Emmerlich; Alexander Goihl; Sabine Wrenger; Ute Bank; Karsten Nordhoff; Michael Täger; Siegfried Ansorge; Dirk Reinhold; Frank Striggow
Journal:  J Neuroinflammation       Date:  2012-02-28       Impact factor: 8.322

5.  Asymmetric synthesis of γ-chloro-α,β-diamino- and β,γ-aziridino-α-aminoacylpyrrolidines and -piperidines via stereoselective Mannich-type additions of N-(diphenylmethylene)glycinamides across α-chloro-N-sulfinylimines.

Authors:  Gert Callebaut; Sven Mangelinckx; Pieter Van der Veken; Karl W Törnroos; Koen Augustyns; Norbert De Kimpe
Journal:  Beilstein J Org Chem       Date:  2012-12-05       Impact factor: 2.883
  5 in total

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